5 research outputs found
Quinine Acesulfamates
Pharmaceutical salts
have been traditionally used in drug formulation.
As a salt former, acesulfame (AH), an aliphatic calorie-free sweetener,
is actively being employed. Acesulfamates of active pharmaceutical
ingredients (APIs) may provide a pleasant sweet taste along with modified
physicochemical properties. In this paper, four quinine (QN) salts
were obtained with AH, including two 1:1 anhydrous forms (QNAH11a
and QNAH11b), one monohydrate of 1:1 salt (QNAH111), and one 1:2 anhydrous
forms (QNAH12). The resulting salts were fully characterized by a
range of analytical methods. Crystal structures of QNAH11a, QNAH111,
and QNAH12 were determined by single-crystal X-ray diffraction, and
the crystal structure of QNAH11b was solved from powder X-ray diffraction
data by Rietveld refinement. Ionization states for all samples were
confirmed by <sup>13</sup>C solid-state NMR spectra. The mutual transformation
and thermodynamic relationships of these solid forms were revealed
via slurry conversion experiments and differential scanning calorimetry
measurements. Additionally, enhanced solubility was observed for each
acesulfamate when compared with the pure free base. This study should
further highlight the potential of AH as a pharmaceutical salt/cocrystal
former